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Assay Detail

CHEMBL700573

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of the binding of radioligand [3H]AMPA in the presence at low-affinity AMPA receptor sites.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate receptor ionotropic AMPA (CHEMBL2096670)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Novel class of amino acid antagonists at non-N-methyl-D-aspartic acid excitatory amino acid receptors. Synthesis, in vitro and in vivo pharmacology, and neuroprotection.
Krogsgaard-Larsen P, Ferkany JW, Nielsen EO, Madsen U, Ebert B, Johansen JS, Diemer NH, Bruhn T, Beattie DT, Curtis DR.
J Med Chem (1991) 34 : 123 -130
PubMed 1825114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.23 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 6.44
CHEMBL291274 1 4.01
CHEMBL1159826 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 364.0 nM 6.44
CHEMBL291274 IC50 = 98000.0 nM 4.01
CHEMBL1159826 IC50 = 335000.0 nM -